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Bismuth-norfloxacin complex: synthesis, physicochemical and antimicrobial evaluation
Anwar R Shaikh1, Rajani Giridhar, Mange Ram Yadav
1Pharmacy Department, Faculty of Technology and Engineering, The M.S. University of Baroda, Vadodara 390 001, India.
International Journal of Pharmaceutics
|December 19, 2006
Summary
A new bismuth complex of norfloxacin (BNC) shows enhanced antibacterial activity against Gram-positive and Gram-negative bacteria. This bismuth-norfloxacin complex may be more effective than norfloxacin alone due to increased bioavailability.
Area of Science:
- Pharmacology
- Medicinal Chemistry
- Microbiology
Background:
- Norfloxacin is a fluoroquinolone antibiotic effective against various bacteria.
- Metal ions can significantly influence the activity of fluoroquinolones.
- Bismuth compounds possess inherent antibacterial properties.
Purpose of the Study:
- To synthesize and characterize a bismuth complex of norfloxacin (BNC).
- To evaluate the antimicrobial efficacy of BNC compared to norfloxacin and a physical mixture.
- To investigate the potential for enhanced antibacterial activity through metal complexation.
Main Methods:
- Synthesis of BNC by reacting bismuth citrate with norfloxacin.
- Structural confirmation using spectral, chemical, and elemental analysis.
- Antimicrobial activity assessment via agar diffusion against selected bacterial strains (E. coli, K. pneumoniae, S. aureus, B. pumilis, S. epidermidis).
Main Results:
- The structure of the bismuth-norfloxacin complex (BNC) was successfully confirmed.
- BNC demonstrated a significant increase in antibacterial activity compared to norfloxacin and a physical mixture (p<0.05).
- Enhanced activity is attributed to the increased bioavailability of the metal-drug complex.
Conclusions:
- The bismuth-norfloxacin complex (BNC) exhibits superior antibacterial efficacy over norfloxacin alone.
- Metal complexation offers a promising strategy to enhance the therapeutic potential of fluoroquinolones.
- BNC represents a potentially more effective therapeutic agent for bacterial infections.
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